64208-32-8

Usage

Uses

CGP 12177 Hydrochloride is a selective β3-adrenoceptor agonist.

Biological Activity

cgp 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors with ki values of 0.9, 4 and 88 nm for β1-, β2- and β3-adrenoceptors, respectively.β3-adrenoceptor is exists mainly in adipose tissue and plays an important role in the regulation of thermogenesis and lipolysis.cgp 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors. in human ventricular myocytes (hvms), cgp12177 slightly activated l-type ca2+ current (ica,l) [1].in sympathectomized (sx) interscapular brown adipose tissue (bat) isolated from rats, cgp-12177 restored normal thyroxine (t4) deiodination, which suggested that cgp-12177 activated 5’-deiodinase type ii through β3-adrenoceptor [2]. in spontaneously hypertensive rats (shr) and normotensive rats, cgp12177 induced vasorelaxant effects and decreased hindquartersperfusion pressure in a dose-dependent way induced by 5-hydroxytryptamine (5-ht), which was inhibited by bupranolol, a β1la-adrenoceptor antagonist. these results suggested that cgp12177 induced vasorelaxant effects through activation of β1la-adrenoceptor [3].

references

[1]. treinys r, zablockait? d, gendvilien? v, et al. β?-adrenergic regulation of l-type ca2? current and force of contraction in human ventricle. j membr biol, 2014, 247(4): 309-318.[2]. hofer d, raíces m, schauenstein k, et al. the in vivo effects of beta-3-receptor agonist cgp-12177 on thyroxine deiodination in cold-exposed, sympathectomized rat brown fat. eur j endocrinol, 2000, 143(2): 273-277.[3]. holopherne d, mallem my, le strat e, et al. cgp12177-induced haemodynamic and vascular effects in normotensive and hypertensive rats. eur j pharmacol, 2008, 591(1-3): 196-202.